CA2397354C - Derives o-methyles de la rapamycine destines a soulager et a inhiber les syndromes lymphoproliferatifs - Google Patents

Derives o-methyles de la rapamycine destines a soulager et a inhiber les syndromes lymphoproliferatifs Download PDF

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Publication number
CA2397354C
CA2397354C CA2397354A CA2397354A CA2397354C CA 2397354 C CA2397354 C CA 2397354C CA 2397354 A CA2397354 A CA 2397354A CA 2397354 A CA2397354 A CA 2397354A CA 2397354 C CA2397354 C CA 2397354C
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Prior art keywords
rapamycin
hydroxy
group
derivative
ethyl
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Expired - Lifetime
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CA2397354A
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CA2397354A1 (fr
Inventor
Mariusz A. Wasik
Leslie M. Shaw
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University of Pennsylvania Penn
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University of Pennsylvania Penn
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    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/5044—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics involving specific cell types
    • G01N33/5047—Cells of the immune system
    • G01N33/5052—Cells of the immune system involving B-cells
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/5011—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing antineoplastic activity

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cell Biology (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biotechnology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Microbiology (AREA)
  • Toxicology (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
CA2397354A 2000-01-14 2001-01-12 Derives o-methyles de la rapamycine destines a soulager et a inhiber les syndromes lymphoproliferatifs Expired - Lifetime CA2397354C (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US17608600P 2000-01-14 2000-01-14
US60/176,086 2000-01-14
PCT/US2001/001537 WO2001051049A1 (fr) 2000-01-14 2001-01-12 Derives o-methyles de la rapamycine destines a soulager et a inhiber les syndromes lymphoproliferatifs

Publications (2)

Publication Number Publication Date
CA2397354A1 CA2397354A1 (fr) 2001-07-19
CA2397354C true CA2397354C (fr) 2011-07-19

Family

ID=22642913

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2397354A Expired - Lifetime CA2397354C (fr) 2000-01-14 2001-01-12 Derives o-methyles de la rapamycine destines a soulager et a inhiber les syndromes lymphoproliferatifs

Country Status (10)

Country Link
US (5) US7754734B2 (fr)
EP (2) EP2298299A3 (fr)
JP (3) JP2003519655A (fr)
AT (1) ATE475418T1 (fr)
AU (2) AU3095601A (fr)
CA (1) CA2397354C (fr)
DE (1) DE60142677D1 (fr)
ES (1) ES2349458T3 (fr)
HK (1) HK1050145A1 (fr)
WO (1) WO2001051049A1 (fr)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6890546B2 (en) * 1998-09-24 2005-05-10 Abbott Laboratories Medical devices containing rapamycin analogs
EP2298299A3 (fr) * 2000-01-14 2012-02-29 The Trustees Of The University Of Pennsylvania Dérivés de rapamycine o-méthylée pour la réduction et l'inhibition du syndrome lymphoprolifératif
PT2269603E (pt) * 2001-02-19 2015-09-09 Novartis Ag Tratamento de tumores da mama com um derivado de rapamicina em combinação com exemestano
AU2011226833B9 (en) * 2001-02-19 2014-07-03 Novartis Ag Cancer treatment
US7682387B2 (en) * 2002-04-24 2010-03-23 Biosensors International Group, Ltd. Drug-delivery endovascular stent and method for treating restenosis
US6939376B2 (en) 2001-11-05 2005-09-06 Sun Biomedical, Ltd. Drug-delivery endovascular stent and method for treating restenosis
US20040024450A1 (en) * 2002-04-24 2004-02-05 Sun Biomedical, Ltd. Drug-delivery endovascular stent and method for treating restenosis
US7169404B2 (en) * 2003-07-30 2007-01-30 Advanced Cardiovasular Systems, Inc. Biologically absorbable coatings for implantable devices and methods for fabricating the same
US7901451B2 (en) 2004-09-24 2011-03-08 Biosensors International Group, Ltd. Drug-delivery endovascular stent and method for treating restenosis
US8067055B2 (en) * 2006-10-20 2011-11-29 Biosensors International Group, Ltd. Drug-delivery endovascular stent and method of use
US20080097591A1 (en) 2006-10-20 2008-04-24 Biosensors International Group Drug-delivery endovascular stent and method of use
US20080103584A1 (en) * 2006-10-25 2008-05-01 Biosensors International Group Temporal Intraluminal Stent, Methods of Making and Using
KR100930167B1 (ko) * 2007-09-19 2009-12-07 삼성전기주식회사 초광각 광학계
WO2009131631A1 (fr) * 2008-04-14 2009-10-29 Poniard Pharmaceuticals, Inc. Analogues de rapamycine en tant qu’agents anti-cancéreux
PT2365802T (pt) 2008-11-11 2017-11-14 Univ Texas Microcápsulas de rapamicina e utilização para o tratamento de cancro
US9283211B1 (en) 2009-11-11 2016-03-15 Rapamycin Holdings, Llc Oral rapamycin preparation and use for stomatitis
WO2015161139A1 (fr) 2014-04-16 2015-10-22 Rapamycin Holdings, Llc Préparation orale de rapamycine et utilisation pour une stomatite
CN102268015B (zh) * 2011-08-30 2013-08-28 成都摩尔生物医药有限公司 一种依维莫司的合成方法
EP2906214A1 (fr) 2012-10-12 2015-08-19 The Board of Regents of The University of Texas System Utilisation d'inhibiteurs mtor pour traiter le déficit cognitif vasculaire
US20160030401A1 (en) 2013-03-13 2016-02-04 The Board Of Regents Of The University Of Texas System Use of mtor inhibitors for prevention of intestinal polyp growth and cancer
US9700544B2 (en) 2013-12-31 2017-07-11 Neal K Vail Oral rapamycin nanoparticle preparations
EP3089737B1 (fr) 2013-12-31 2021-11-03 Rapamycin Holdings, LLC Préparations orales de nanoparticules de rapamycine, et utilisation
CN105254646A (zh) * 2014-05-28 2016-01-20 上海博邦医药科技有限公司 一种制备依维莫司的方法
WO2016117431A1 (fr) * 2015-01-19 2016-07-28 学校法人慶應義塾 Agent thérapeutique pour perte d'audition neurosensorielle
EP3576736A4 (fr) * 2017-02-10 2020-08-26 Torcept Therapeutics Inc. Analogue de rapamycine
EP3624863B1 (fr) 2017-05-15 2021-04-14 C.R. Bard, Inc. Dispositif médical à revêtement d'élution de médicament et à couche intermédiaire
CN113226389B (zh) 2018-11-14 2022-11-08 乐通公司 在经改性设备表面上具有药物洗脱涂层的医疗设备
CN109776571B (zh) * 2019-01-31 2021-06-11 哈药慈航制药股份有限公司 一种雷帕霉素类似物及其制备方法和应用
WO2020209828A1 (fr) 2019-04-08 2020-10-15 Bard Peripheral Vascular, Inc. Dispositif médical portant un revêtement d'élution de médicament sur une surface modifiée de dispositif
CN110917194A (zh) * 2019-11-07 2020-03-27 福建省微生物研究所 雷帕霉素噻唑类衍生物在制备抗阿尔茨海默症药物中的应用
CN115323915B (zh) * 2022-10-17 2023-01-06 广州市市政工程试验检测有限公司 一种桥梁索杆检测与修复机器人

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5206018A (en) * 1978-11-03 1993-04-27 Ayerst, Mckenna & Harrison, Inc. Use of rapamycin in treatment of tumors
US4401653A (en) * 1981-03-09 1983-08-30 Ayerst, Mckenna & Harrison Inc. Combination of rapamycin and picibanil for the treatment of tumors
US4699783A (en) * 1983-03-11 1987-10-13 Terman David S Products and methods for treatment of cancer
DE69209183T2 (de) * 1991-06-18 1996-08-08 American Home Prod Verwendung von Rapamycin zur Behandlung von T-Zellen Lymphom/Leukämie bei Erwachsenen
GB9221220D0 (en) * 1992-10-09 1992-11-25 Sandoz Ag Organic componds
US5258389A (en) * 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
US5527907A (en) * 1993-11-19 1996-06-18 Abbott Laboratories Macrolide immunomodulators
US5525610A (en) * 1994-03-31 1996-06-11 American Home Products Corporation 42-Epi-rapamycin and pharmaceutical compositions thereof
EP0896544B1 (fr) * 1996-06-11 2003-02-26 Novartis AG Association d'un analogue de somatostatine et d'une rapamycine
JP3352411B2 (ja) * 1998-03-05 2002-12-03 株式会社東芝 制御システム、電力系統保護制御システムおよびプログラムを記憶した記憶媒体
AU4565000A (en) 1999-05-10 2000-11-21 Novartis Ag Organic compounds
EP2298299A3 (fr) * 2000-01-14 2012-02-29 The Trustees Of The University Of Pennsylvania Dérivés de rapamycine o-méthylée pour la réduction et l'inhibition du syndrome lymphoprolifératif
JP2004509898A (ja) * 2000-09-19 2004-04-02 ワイス 水溶性ラパマイシンエステル
US6399625B1 (en) * 2000-09-27 2002-06-04 Wyeth 1-oxorapamycins
US6399626B1 (en) * 2000-10-02 2002-06-04 Wyeth Hydroxyesters of 7-desmethylrapamycin
US6440991B1 (en) * 2000-10-02 2002-08-27 Wyeth Ethers of 7-desmethlrapamycin

Also Published As

Publication number Publication date
JP2010090131A (ja) 2010-04-22
US20100305151A1 (en) 2010-12-02
US7781447B2 (en) 2010-08-24
US8569332B2 (en) 2013-10-29
HK1050145A1 (en) 2003-06-13
US8759370B2 (en) 2014-06-24
EP2298299A3 (fr) 2012-02-29
US7754734B2 (en) 2010-07-13
US20110104304A1 (en) 2011-05-05
AU3095601A (en) 2001-07-24
US20100290994A1 (en) 2010-11-18
EP1250135A1 (fr) 2002-10-23
JP2003519655A (ja) 2003-06-24
EP1250135A4 (fr) 2006-06-07
US8778961B2 (en) 2014-07-15
JP5184894B2 (ja) 2013-04-17
EP2298299A2 (fr) 2011-03-23
US20080125457A1 (en) 2008-05-29
US20040010002A1 (en) 2004-01-15
CA2397354A1 (fr) 2001-07-19
WO2001051049A1 (fr) 2001-07-19
EP1250135B1 (fr) 2010-07-28
DE60142677D1 (de) 2010-09-09
JP5180177B2 (ja) 2013-04-10
WO2001051049A9 (fr) 2003-01-16
ATE475418T1 (de) 2010-08-15
ES2349458T3 (es) 2011-01-03
US20080182867A9 (en) 2008-07-31
JP2008106074A (ja) 2008-05-08
AU2001230956B2 (en) 2005-08-18

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